Pharmacological study of a new anti-inflammatory steroid, tixocortol pivalate (JO 1016).
Some pharmacological activities of pregn-4-ene-3,20-dione-21-thiol-11 beta,17 alpha-dihydroxy-21-pivalate (tixocortol pivalate, JO 1016 Pivalone), a new steroidal anti-inflammatory compound, are described. The anti-inflammatory activity of tixocortol pivalate has been clearly demonstrated in various tests using adrenalectomised and intact animals. Of particular interest is the dissociation of its local and systemic activities. Comparison with hydrocortisone acetate indicates a similar or greater anti-inflammatory activity, by either the local or topical routes, but tixocortol pivalate is between 60 and 300 times less active than hydrocortisone acetate after oral or subcutaneous administration. Glucocorticoid activity was only detected at very high oral doses of tixocortol pivalate and the highest tested subcutaneous dose (300 mg/kg) failed to induce significant activity. Hydrocortisone acetate exerted glucocorticoid effects at much lower doses. It is possible therefore the local or topical use of tixocortol pivalate in therapy may not cause the unwanted side effects of many of the corticosteroids in current use.
D000284:Administration, Oral; D000315:Adrenalectomy; D000523:Algestone / Q000031:analogs & derivatives* / Q000494:pharmacology; D000463:Algestone Acetophenide / Q000031:analogs & derivatives*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D005938:Glucocorticoids; D006003:Glycogen / Q000378:metabolism; D006128:Growth / Q000187:drug effects; D006854:Hydrocortisone / Q000494:pharmacology / Q000031:analogs & derivatives; D007279:Injections, Subcutaneous; D008297:Male; D051381:Rats; D013950:Thymus Gland / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D000523:Algestone; C019112:tixocortol pivalate; D006003:Glycogen; D000463:Algestone Acetophenide; D006854:Hydrocortisone